Date published: 2025-12-10

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BRD4 Inhibitors

BRD4 inhibitors represent a class of chemical compounds strategically designed to target and inhibit the bromodomain-containing protein 4 (BRD4), a crucial epigenetic regulator intricately involved in the complex orchestration of transcriptional processes and chromatin remodeling within cells. The key modus operandi of these inhibitors lies in their capacity to disrupt the pivotal interaction between BRD4 and acetylated histones, thereby impeding the binding of BRD4 to chromatin and subsequent modulation of gene expression. At the molecular level, BRD4 is distinguished by its possession of two bromodomains, specialized regions adept at recognizing acetyl-lysine residues on histones. This unique structural feature allows BRD4 to serve as a molecular scaffold for the assembly of transcriptional complexes, facilitating the intricate choreography of gene expression. The precise and selective binding of BRD4 inhibitors to the bromodomains of BRD4 precludes the recruitment of BRD4 to chromatin, thereby thwarting its capacity to govern transcriptional activity. This interference manifests as a disruptive force in the finely tuned mechanisms of gene regulation, with potential repercussions spanning diverse cellular processes such as cell cycle progression, cellular differentiation, and the regulation of inflammatory responses. The burgeoning interest and active pursuit of research in the development of BRD4 inhibitors underscore the anticipation of their far-reaching implications in the modulation of cellular behavior. The intricate interplay between BRD4 and the epigenetic landscape make these inhibitors promising candidates for unraveling the complexities of gene regulation. The evolving understanding of BRD4's role in the intricate dance of cellular processes positions BRD4 inhibitors as valuable tools in deciphering the nuanced language of gene expression and uncovering novel strategies for manipulating cellular behavior.
Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

PFI-1

1403764-72-6sc-478504
5 mg
$96.00
(0)

PFI-1 is a potent inhibitor of BRD4, distinguished by its unique ability to modulate chromatin dynamics. It selectively targets the bromodomain, engaging in specific π-π stacking interactions that enhance binding specificity. The compound's rigid scaffold promotes a stable conformation, optimizing its interaction with the target. Furthermore, PFI-1 exhibits favorable kinetic properties, allowing for rapid association and dissociation rates, which are crucial for effective modulation of transcriptional regulation.

(±)-JQ1

1268524-69-1sc-472932
sc-472932A
5 mg
25 mg
$226.00
$846.00
1
(0)

(±)-JQ1 is a selective inhibitor of the bromodomain-containing protein BRD4, characterized by its ability to disrupt protein-protein interactions through a unique binding mechanism. The compound engages in hydrogen bonding and hydrophobic interactions, stabilizing its complex with BRD4. Its structural flexibility allows for diverse conformational states, enhancing its binding affinity. Additionally, the compound's solubility properties facilitate its distribution in biological systems, promoting effective target engagement.

(S)-2-(4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(4-hydroxyphenyl)acetamide

202590-98-5sc-501130
2.5 mg
$330.00
(0)

(S)-2-(4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(4-hydroxyphenyl)acetamide (OTX-015) is a small molecule inhibitor that targets BRD2, BRD3, and BRDIt has shown promising anti-tumor activity in research studies and has been investigated in investigated for various cancers.

CPI-203

1446144-04-2sc-501599
1 mg
$170.00
(0)

CPI-203 is a selective small molecule inhibitor of BRD4 that has demonstrated anti-proliferative effects in cancer cells. It can inhibit BRD4-mediated transcription and has been evaluated in reserach models for hematological malignancies.

4-[(1E)-2-(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-N-2-pyridinylbenzenesulfonamide

1395084-25-9sc-480120
5 mg
$300.00
(0)

4-[(1E)-2-(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-N-2-pyridinylbenzenesulfonamide (MS436), is a potent small molecule inhibitor that targets the bromodomains of BRD4 and BRDIt has demonstrated anti-proliferative effects in cancer cells and has been studied for its potential as an anti-cancer therapy.